pcc

PCC0208017 is an inhibitor of MARK3 and MARK4 with IC50s of 1.8 and 2.01 nM. PCC0208017 disrupts microtubule dynamics and displays potent antitumor activity.

PCC0208018 is a novel activator of effector T cells, enhancing T cell proliferation and activation to release interferon gamma (IFN-γ) and interleukin-2 (IL-2) without blocking the programmed cell death 1 (PD-1)/programmed cell death-ligand 1 (PD-L1) binding and not directly affecting tumor cell viability in vitro.

YUN90389, also known as PPARalpha/delta-IN-11, is a the first reported pparα/δ dual antagonist. YUN90389 was first reported in Bioorganic & Medicinal Chemistry Letters (2019), 29(3), 503-508. YUN90389 has CAS#1673590-38-9. This product has no formal name at the moment. For the convenience of communication, a temporary code name was therefore proposed according to MedKoo Chemical Nomenclature (see web page: https://www.medkoo.com/page/naming).

PCC16 chloride, a CRBN-based cp-PCC, exhibits an IC50 of 102 nM for the degradation of DHHC3. This compound also demonstrates antitumor activity.

PCC0208009 (IDO-IN-2) is an IDO inhibitor.

PCC0105003 is an effective inhibitor of MARK. This compound is utilized in the study of neuropathic pain.

Procyanidin C1 is a natural polyphenol that causes DNA damage, cell cycle arrest, and apoptosis induction. It reduces Bcl-2 protein levels and enhances the expression of BAX, caspase 3, and 9 in cancer cells.

(1R,2R)-2-PCCA hydrochloride is a potent, selective, and blood-brain-barrier-crossing GPR88 receptor agonist with an EC50 value of 1140 n in striatal membranes of WT mice; it can be used to study the central nervous system.

(1S,2R)-2-PCCA is a novel and potent small molecule GPR88 receptor agonist with an EC50 value of 3 nM in the non-cellular system and 603 nM in the cellular system.

2-PCCA hydrochloride, a racemate, is a potent and selective GPR88 receptor agonist showing inhibition of GPR88-mediated cAMP production in HEK293 cells with an EC50 value of 116 nM.

CPCCOEt is a low-affinity, selective, non-competitive, and reversible antagonist of mGluR1b.

DHPCC-9 is an inhibitor of Pim kinase.

(±)-PPCC is a sigma-1 agonist that interacts with sigma-1 receptors (Ki=1.5 nM). (±)-PPCC has anti-amnestic effects in rats with cognitive impairment and can improve cognitive abilities in rats.

Selective sigma (σ) receptor ligand. Displays high affinity for σ1; also binds at σ2 sites (Ki = 1.5 nM and 50.8 nM respectively). Selective over a range of receptor types including dopaminergic and muscarinic receptors, DAT and SERT. Prezzavento et al (2007) Novel sigma receptor ligands: synthesis and biological profile. J.Med.Chem. 50 951 PMID:17328523 |Prezzavento et al (2008) A new sigma ligand, (±)-PPCC, antagonizes kappa opioid receptor-mediated antinociceptive effect. Life Sci. 82 549 PMID:18261749 |Antonini et al (2009) Anti-amnesic properties of (±)-PPCC, a novel sigma receptor ligand, on cognitive dysfunction induced by selective cholinergic lesion in rats. J.Neurochem. 109 744 PMID:19245662

2-PCCA is a GPR88 agonist.

(±)-PPCC oxalate, a sigma-1 agonist with a K i of 1.5 nM, primarily targets sigma-1 receptors and exhibits significant anti-amnesia effects in rats with mild or severe cognitive impairment, enhancing their cognitive abilities [1].

TASIN-1 Hydrochloride (TASIN-1 HCl) is a selective inhibitor of truncated APC that acts by selectively killing colorectal cancer cells that express truncated APC by reducing cellular cholesterol levels and inducing apoptotic cell death through the ER stress/ROS/JNK signaling in colon cancer cells.

ProTAME is an inhibitor of APC/CFzr and APC/CCdc20. Combinations of proTAME with topoisomerase inhibitors, doxorubicin and etoposide, significantly increase cell death in primary cells and Multiple Myeloma (MM) cell lines, particularly if TOPIIα levels are first increased through pre-treatment with ProTAME.This compound is unstable in powder form and other related salt forms are recommended.

TAME hydrochloride (Tos-Arg-OMe HCl) is a kind od amino acid derivatives.

CFM 4 is a potent small molecule CARP-1/APC-2 antagonist that prevents CARP-1 from binding to APC-2, contributes to G2M cell cycle arrest, and induces apoptosis, with an IC50 in the range of 10-15 μM.CFM 4 inhibits the growth of drug-resistant human breast cancer cells.

Apcin-A is an anaphase-promoting complex (APC) inhibitor. It interacts strongly with Cdc20 and inhibits the ubiquitination of Cdc20 substrates. Apcin-A can be used to synthesize the PROTAC CP5V.

CP5V is a rationally designed PROTAC molecule composed of ligands for von Hippel–Lindau and cyclin-dependent kinase, which selectively induces degradation of Cdc20 by tethering it to the VHL/VBC E3 ligase complex, leading to ubiquitination and proteasomal degradation, mitotic arrest, and suppression of cancer cell proliferation, thereby serving as a mechanistic tool for cell cycle and oncology research.

Unesbulin (PTC596) is an orally active, selective inhibitor of B-cell-specific Moloney murine leukemia virus integration site 1 (BMI-1).

(S,R,S)-AHPC-C10-NH2 (VH032-C10-NH2) is a synthesized E3 ligase ligand-linker conjugate, comprising an (S,R,S)-AHPC-based VHL ligand and a linker, designed for BET-targeted PROTAC applications.